PVTX-405

PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50 of 0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn391V C57BL/6 mice[1].

Product Specifications

CAS Number

[2991021-08-8]

UNSPSC

12352005

Target

IKZF Family; Molecular Glues; Potassium Channel

Related Pathways

Immunology/Inflammation; Membrane Transporter/Ion Channel; PROTAC

Applications

COVID-19-immunoregulation

Field of Research

Cancer; Inflammation/Immunology

Smiles

O=C1C2=CC=C(C(OC3)=C2CN1[C@@H]4C(NC(CC4)=O)=O)C3(CC5)CCN5CC6=CC(C7=CN(N=C7)C)=CC=C6

Molecular Formula

C30H31N5O4

Molecular Weight

525.60

References & Citations

[1]Chen X, et al. Design, synthesis, and biological evaluation of N- (2-amino-phenyl) -5- (4-aryl-pyrimidin-2-yl) amino) -1H-indole-2-carboxamide derivatives as novel inhibitors of CDK9 and class I HDACs for cancer treatment [J]. Bioorganic Chemistry, 2025: 108577.